NYX-2925

产品编号: DC11382 Featured
NYX-2925
结构式
2012536-16-0
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中国地区超过5000个高品质化合物库存
应用领域
NYX-2925是一种新型NMDA受体特异性螺环-β-内酰胺,可调节与学习和记忆相关的突触可塑性过程。
Cas No.: 2012536-16-0
名称: (2S,3R)-3-hydroxy-2-((R)-5-isobutyryl-1-oxo-2,5-diazaspiro[3.4]octan-2-yl)butanamide
别名: NYX-2925,NYX 2925,NYX2925
SMILES: C1CCN(C(=O)C(C)C)[C@@]11C(=O)N([C@H]([C@@H](O)C)C(=O)N)C1
分子式: C14H23N3O4
分子量: 297.35
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: NYX-2925 has a low potential for "off-target" activity, as it did not exhibit any significant affinity for a large panel of neuroactive receptors, including hERG receptors. NYX-2925 increased MK-801 binding to human N-methyl-D-aspartate receptor NR2A-D subtypes expressed in HEK cells and enhanced N-methyl-D-aspartate receptor current and long-term potentiation (LTP) in rat hippocampal slices (100-500 nM). Single dose ex vivo studies showed increased metaplasticity in a hippocampal LTP paradigm and structural plasticity 24 hours after administration (1 mg/kg p.o.). Significant learning enhancement in both novel object recognition and positive emotional learning paradigms were observed (0.01-1 mg/kg p.o.), and these effects were blocked by the N-methyl-D-aspartate receptor antagonist CPP. NYX-2925 does not show any addictive or sedative/ataxic side effects and has a therapeutic index of >1000. NYX-2925 (1 mg/kg p.o.) has a cerebrospinal fluid half-life of 1.2 hours with a Cmax of 44 nM at 1 hour.NYX-2925, like rapastinel, activates an NMDA receptor-mediated synaptic plasticity process and may have therapeutic potential for a variety of NMDA receptor-mediated central nervous system disorders.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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MSDS_742_DC11382_2012536-16-0
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